Skip to main content
SpringerLink
Log in

Capsaicin-Based Therapies for Pain Control

  • Chapter
  • First Online:
Capsaicin as a Therapeutic Molecule

Part of the book series: Progress in Drug Research ((PDR,volume 68))

Abstract

The TRPV1 receptor is known to play a role in nociceptive transmission in multiple organ systems, usually in response to the pain of inflammation. TRPV1 antagonism has so far shown limited benefit in antinociception. Capsaicin, a TRPV1 agonist, has been shown to induce a refractory period in the nerve terminal expressing TRPV1 and even, in sufficient dosing, to create long-term nerve terminal defunctionalization. This has led to research into topical capsaicin as a treatment for multiple painful conditions. The majority of work has focused on musculoskeletal pain and neuropathic pain and has revealed that although low-dose topical capsaicin has limited effectiveness as an analgesic, high-dose capsaicin, when tolerated, has the potential for long-term analgesia in certain types of neuropathic pain.

Howard Smith—deceased

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 129.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Hardcover Book
USD 169.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  • Adcock JJ (2009) TRPV1 receptors in sensitisation of cough and pain reflexes. Pulm Pharmacol Ther 22:65–70. doi:10.1016/j.pupt.2008

    Article  CAS  PubMed  Google Scholar 

  • Anand P, Bley K (2011) Topical capsaicin for pain management: therapeutic potential and mechanisms of action of the new high-concentration capsaicin 8 % patch. Br J Anaesth 107:490–502. doi:10.1093/bja/aer260

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Argoff CE (2011) Review of current guidelines on the care of postherpetic neuralgia. Postgrad Med 123:134–142. doi:10.3810/pgm.2011.09.2469

    Article  PubMed  Google Scholar 

  • Bevan S, Szolcsányi J (1990) Sensory neuron-specific actions of capsaicin: mechanisms and applications. Trends Pharmacol Sci 11:330–333

    Article  CAS  PubMed  Google Scholar 

  • Brederson JD, Kym PR, Szallasi A (2013) Targeting TRP channels for pain relief. Eur J Pharmacol doi:pii: S0014-2999(13)00173-8. 10.1016/j.ejphar.2013.03.003

  • Cao E, Cordero-Morales JF, Liu B, Qin F, Julius D (2013) TRPV1 channels are intrinsically heat sensitiveand negatively regulated by phosphoinositide lipids. Neuron 77:667–679. doi:10.1016/j.neuron.2012.12.016

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Casanueva B, Rodero B, Quintial C, Llorca J, González-Gay MA (2013) Short term efficacy of topical capsaicin therapy in severely affected fibromyalgia patients. Rheumatol Int 33(10):2665–2670

    Google Scholar 

  • Caterina MJ, Schumacher MA, Tominaga M, Rosen TA, Levine JD, Julius D (1997) The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 389:816–824

    Article  CAS  PubMed  Google Scholar 

  • Chang HC, Chen ST, Chien SY, Kuo SJ, Tsai HT, Chen DR (2011) Capsaicin may induce breast cancer cell death through apoptosis-inducing factor involving mitochondrial dysfunction. Hum Exp Toxicol 30:1657–1665. doi:10.1177/0960327110396530

    Article  CAS  PubMed  Google Scholar 

  • Chizh BA, O’Donnell MB, Napolitano A, Wang J, Brooke AC, Aylott MC, Bullman JN, Gray EJ, Lai RY, Williams PM, Appleby JM (2007) The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor mediated activity and inflammatory hyperalgesia in humans. Pain 132:132–141

    Article  CAS  PubMed  Google Scholar 

  • Cianchetti C (2010) Capsaicin jelly against migraine pain. Int J Clin Pract 64:457–459. doi:10.1111/j.1742-1241.2009.02294.x

    Article  CAS  PubMed  Google Scholar 

  • Clifford DB, Simpson DM, Brown S (2012) A randomized, double-blind, controlled study of NGX-4010, a capsaicin 8 % Dermal patch, for the treatment of painful HIV-associated distal sensory polyneuropathy. J Acquir Immune Defic Syndr 59:126–133. doi:10.1097/QAI.0b013e31823e31f7

    Article  CAS  PubMed  Google Scholar 

  • Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, Chandran P, Gomtsyan A, Brown B, Bayburt EK, Marsh K, Bianchi B, McDonald H, Niforatos W, Neelands TR, Moreland RB, Decker MW, Lee CH, Sullivan JP, Faltynek CR (2006) TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J Neurosci 26:9385–9393

    Article  CAS  PubMed  Google Scholar 

  • Davis JB, Gray J, Gunthorpe MJ, Hatcher JP, Davey PT, Overend P, Harries MH, Latcham J, Clapham C, Atkinson K, Hughes SA, Rance K, Grau E, Harper AJ, Pugh PL, Rogers DC, Bingham S, Randall A, Sheardown SA (2000) Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia. Nature 405:183–187

    Google Scholar 

  • Derry S, Moore RA (2012) Topical capsaicin (low concentration) for chronic neuropathic pain in adults. Cochrane Database Syst Rev 9:CD010111. doi:10.1002/14651858.CD010111

  • Derry S, Lloyd R, Moore RA, McQuay HJ (2009) Topical capsaicin for chronic neuropathic pain in adults. Cochrane Database Syst Rev (4):CD007393. doi:10.1002/14651858.CD007393.pub2

  • Dworkin RH, O’Connor AB, Audette J, Baron R, Gourlay GK, Haanpää ML, Kent JL, Krane EJ, LeBel AA, Levy RM, Mackey SC, Mayer J, Miaskowski C, Raja SN, Rice ASC, Schmader KE, Stacey B, Stanos S, Treede RD, Turk DC, Walco CA, Wells CD (2010) Recommendations for the pharmacological management of neuropathic pain: an overview and literature update. Mayo Clin Proc 85:S3–S14. doi:10.4065/mcp.2009.0649

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Engler A, Aeschlimann A, Simmen BR, Michel BA, Gay RE, Gay S, Sprott H (2007) Expression of transient receptor potential vanilloid 1 (TRPV1) in synovial fibroblasts from patients with osteoarthritisand rheumatoid arthritis. Biochem Biophys Res Commun 359:884–888

    Article  CAS  PubMed  Google Scholar 

  • Gavva NR, Treanor JJS, Garami A, Fang L, Surapaneni S, Akrami A, Alvarez F, Bak A, Darling M, Gore A, Jang GR, Kesslak JP, Ni L, Norman MH, Palluconi G, Rose MJ, Salfi M, Tan E, Romanovsky AA, Banfield C, Davar G (2008) Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. Pain 136:202–210. doi:10.1016/j.pain.2008.01.024

    Article  CAS  PubMed  Google Scholar 

  • Haanpää M, Treede RD (2012) Capsaicin for neuropathic pain: linking traditional medicine and molecular biology. Eur Neurol 68:264–275. doi:10.1159/000339944

    Article  PubMed  Google Scholar 

  • Huang D, Li S, Dhaka A, Story GM, Cao YQ (2012) Expression of the transient receptor potential channels TRPV1, TRPA1 and TRPM8 in mouse trigeminal primary afferent neurons innervating the dura. Mol Pain 8:66. doi:10.1186/1744-8069-8-66

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Hutchinson MR, Buijs M, Tuke J, Kwok YH, Gentgall M, Williams D, Rolan P (2013) Low-dose endotoxin potentiates capsaicin-induced pain in man: Evidence for a pain neuroimmune connection. Brain Behav Immun pii:S0889–1591(13)00131-1. doi:10.1016/j.bbi.2013.03.002

  • Immke David C, Gavva Narender R (2006) The TRPV1 receptor and nociception. Semin Cell Dev Biol 17:582–591

    Article  CAS  PubMed  Google Scholar 

  • Khairatkar-Joshi N, Szallasi A (2009) TRPV1 antagonists: the challenges for therapeutic targeting. Trends Mol Med 15:14–22. doi:10.1016/j.molmed.2008.11.004

    Article  CAS  PubMed  Google Scholar 

  • Lambert GA, Davis JB, Appleby JM, Chizh BA, Hoskin KL, Zagami AS (2009) The effects of the TRPV1 receptor antagonist SB-705498 on trigeminovascular sensitisation and neurotransmission. Naunyn Schmiedebergs Arch Pharmacol 380:311–325. doi:10.1007/s00210-009-0437-5

    Article  CAS  PubMed  Google Scholar 

  • Li Q (2012) Antagonists of toll like receptor 4 maybe a new strategy to counteract opioid-induced hyperalgesia and opioid tolerance. Med Hypotheses 79:754–756. doi:10.1016/j.mehy.2012.08.021

    Article  CAS  PubMed  Google Scholar 

  • Liddle RA (2007) The role of transient receptor potential vanilloid 1 (TRPV1) channels in pancreatitis. Biochim Biophys Acta 1772:869–878

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Mason L, Moore RA, Derry S, Edwards JE, McQuay HJ (2004) Systematic review of topical capsaicin for the treatment of chronic pain. BMJ 328:991

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • McCleane G (2003) Pharmacological management of neuropathic pain. CNS Drugs 17:1031–1043

    Article  CAS  PubMed  Google Scholar 

  • Nagy I, Sántha P, Jancsó G, Urbán L (2004) The role of the vanilloid (capsaicin) receptor (TRPV1) in physiology and pathology. Eur J Pharmacol 500:351–369

    Article  CAS  PubMed  Google Scholar 

  • Nilius B (2007) TRP channels in disease. Biochim Biophys Acta 1772:805–812

    Article  CAS  PubMed  Google Scholar 

  • NICE Clinical Guideline 96 (2010) Neuropathic pain: The pharmacological management of neuropathic pain in adults in non-specialist settings. Issued: March 2010. National Institute for Health and Clinical Excellence. http://www.nice.org.uk/guidance/CG96. Accessed 24 April 2013

  • Premkumar LS, Abooj M (2013) TRP channels and analgesia. Life Sci 92:415–424. doi:10.1016/j.lfs.2012.08.010

    Article  CAS  PubMed  Google Scholar 

  • Qutenza Prescribing Information (2009) Copyright 2009 NeurogesX

    Google Scholar 

  • Richards BL, Whittle SL, Buchbinder R (2012) Neuromodulators for pain management in rheumatoid arthritis. Cochrane Database Syst Rev 1:CD008921. doi:10.1002/14651858.CD008921.pub2

  • Ro JY, Lee JS, Zhang Y (2009) Activation of TRPV1 and TRPA1 leads to muscle nociception and mechanical hyperalgesia. Pain 144:270–277. doi:10.1016/j.pain.2009.04.021

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Robbins WR, Staats PS, Levine J, Fields HL, Allen RW, Campbell JN, Pappagallo M (1998) Treatment of intractable pain with topical large-dose capsaicin: preliminary report. Anesth Analg 86(3):579–583

    Google Scholar 

  • Rowbotham MC, Nothaft W, Duan WR, Wang Y, Faltynek C, McGaraughty S, Chu KL, Svensson P (2011) Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Pain 152:1192–1200. doi:10.1016/j.pain.2011.01.051

    Article  CAS  PubMed  Google Scholar 

  • Sayanlar J, Guleyupoglu N, Portenoy R, Ashina S (2012) Trigeminal postherpetic neuralgia responsive to treatment with capsaicin 8 % topical patch: a case report. J Headache Pain 13:587–589. doi:10.1007/s10194-012-0467-0

    Article  PubMed Central  PubMed  Google Scholar 

  • Schwartz ES, Christianson JA, LA Jun-Ho XC, Davis BM, Albers KM, Gebhart GF (2011) Synergistic role of TRPV1 and TRPA1 in pancreatic pain and inflammation. Gastroenterology 140:1283–1291. doi:10.1053/j.gastro.2010.12.033

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Simpson DM, Estanislao L, Brown SJ, Sampson J (2008) An open-label pilot study of high-concentration capsaicin patch in painful HIV neuropathy. J Pain Symptom Manage 35:299–306

    Article  CAS  PubMed  Google Scholar 

  • Summ O, Holland PR, Akerman S, Goadsby PJ (2011) TRPV1 receptor blockade is ineffective in different in vivo models of migraine. Cephalalgia 31:172–180. doi:10.1177/0333102410375626

    Article  PubMed  Google Scholar 

  • Takemura M, Quarcoo D, Niimi A, Dinh QT, Geppetti P, Fischer A, Chung KF, Groneberg DA (2008) Is TRPV1 a useful target in respiratory diseases? Pulm Pharmacol Ther 21:833–839. doi:10.1016/j.pupt.2008.09.005

    Article  CAS  PubMed  Google Scholar 

  • Terenzi R, Romano E, Manetti M, Peruzzi F, Niacci F, Matucci-Cerinic M, Guiducci S (2013) Neuropeptides activate TRPV1 in rheumatoid arthritis fibroblast-like synoviocytes and foster IL-6 and IL-8 production. Ann Rheum Dis 72(6):1107–1109

    Google Scholar 

  • Tominaga M, Tominaga T (2005) Structure and function of TRPV1. Pflugers Arch 451:143–150

    Article  CAS  PubMed  Google Scholar 

  • Vardanyan A, Wang R, Vanderah TW, Ossipov MH, Lai J, Porreca F, King T (2009) TRPV1 receptor in expression of opioid-induced hyperalgesia. J Pain 10:243–252. doi:10.1016/j.jpain.2008.07.004

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Webster LR, Nunez M, Tark MD, Dunteman ED, Lu B, Tobias JK, Vanhove GF (2011) Tolerability of NGX-4010, a capsaicin 8 % dermal patch, following pretreatment with lidocaine 2.5 %/prilocaine 2.5 % cream in patients with postherpetic neuralgia. BMC Anesthesiol 11:25. doi:10.1186/1471-2253-11-25

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Webster LR, Peppin JF, Murphy FT, Tobias JK, Vanhove GF (2012) Tolerability of NGX-4010, a capsaicin 8 % patch, in conjunction with three topical anesthetic formulations for the treatment of neuropathic pain. J Pain Res 5:7–13. doi:10.2147/JPR.S25272

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Wong GY, Gavva NR (2009) Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: recent advances and setbacks. Brain Res Rev 60:267–277. doi:10.1016/j.brainresrev.2008.12.006

    Article  CAS  PubMed  Google Scholar 

  • Zhu Y, Colak T, Shenoy M, Liu L, Pai R, Li C, Mehta K, Pasricha PJ (2011) Nerve growth factor modulates TRPV1 expression and function and mediates pain in chronic pancreatitis. Gastroenterology 141:370–377. doi:10.1053/j.gastro.2011.03.046

    Article  CAS  PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Anesthesiology, Albany Medical College, 47 New Scotland Avenue, MC-131, Albany, NY, 12208, USA

    Howard Smith & John R. Brooks

Authors
  1. Howard Smith
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. John R. Brooks
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to John R. Brooks .

Editor information

Editors and Affiliations

  1. Department of Toxicology and Narcotics, National Research Center, Cairo, Egypt

    Omar M. E. Abdel-Salam

Rights and permissions

Reprints and permissions

Copyright information

© 2014 Springer Basel

About this chapter

Cite this chapter

Smith, H., Brooks, J.R. (2014). Capsaicin-Based Therapies for Pain Control. In: Abdel-Salam, O. (eds) Capsaicin as a Therapeutic Molecule. Progress in Drug Research, vol 68. Springer, Basel. https://doi.org/10.1007/978-3-0348-0828-6_5

Download citation

Publish with us

Policies and ethics

Search

Navigation